Assay Detail
Binding
CHEMBL647547
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]prazosin from Alpha-1A adrenergic receptor of rat submaxillary gland membranes
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Studies on quinazolines and 1,2,4-benzothiadiazine 1,1-dioxides. 8.1, 2 synthesis and pharmacological evaluation of tricyclic fused quinazolines and 1,2,4-benzothiadiazine 1,1-dioxides as potential alpha1-adrenoceptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 8 | 8.72 | 9.64 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1788222 | — | — | 1 | 9.64 |
| CHEMBL106737 | — | — | 1 | 9.59 |
| CHEMBL51433 | — | — | 1 | 9.30 |
| CHEMBL302021 | — | — | 1 | 9.19 |
| CHEMBL1744044 | — | — | 1 | 9.03 |
| CHEMBL1788223 | — | — | 1 | 8.82 |
| CHEMBL2092926 | — | — | 1 | 7.26 |
| CHEMBL2092927 | — | — | 1 | 6.91 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1788222 | — | Ki | = | 0.23 | nM | 9.64 |
| CHEMBL106737 | — | Ki | = | 0.26 | nM | 9.59 |
| CHEMBL51433 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL302021 | — | Ki | = | 0.65 | nM | 9.19 |
| CHEMBL1744044 | — | Ki | = | 0.93 | nM | 9.03 |
| CHEMBL1788223 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL2092926 | — | Ki | = | 55.0 | nM | 7.26 |
| CHEMBL2092927 | — | Ki | = | 122.0 | nM | 6.91 |